MT-DADMe-ImmA (Methylthio-DADMe-Immucillin A)
(Synonyms: MTDIA; Methylthio-DADMe-Immucillin A) 目录号 : GC32730
An MTAP inhibitor
Cas No.:653592-04-2
Sample solution is provided at 25 µL, 10mM.
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MT-DADMe-ImmA is an inhibitor of 5'-methylthioadenosine phosphorylase (MTAP; Ki = 1.7 nM).1 It increases levels of MTA , a product of polyamine metabolism, in FaDu human squamous cell carcinoma cells when used at a concentration of 1 ?M.2 MT-DADMe-ImmA (5, 9, and 21 mg/kg per day for 28 days) reduces tumor growth in a FaDu mouse xenograft model.
1.Evans, G.B., Furneaux, R.H., Lenz, D.H., et al.Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylaseJ. Med. Chem.48(14)4679-4689(2005) 2.Basu, I., Cordovano, G., Das, I., et al.A transition state analogue of 5'-methylthioadenosine phosphorylase induces apoptosis in head and neck cancersJ. Biol. Chem.282(29)21477-21486(2007)
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Cell experiment: |
Cell viability is evaluated using the Alamar Blue assay. Cells are seeded onto 96-well plates at a density of 104 cells/well and incubated with increasing concentrations of MT-DADMe-ImmA (100 pM to 100 μM) for 4 days at fixed MTA concentrations (0, 5, 10, and 20 μM). IC50 is determined with the assay data[2]. |
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Animal experiment: |
Mice: Tumors were established in mice for 5 days prior to oral or intraperitoneal treatments with MT-DADMe-ImmA. Mice are treated with oral dose of 21 mg/kg or an intraperitoneal dose of 5 mg/kg/day MT-DADMe-ImmA[2]. |
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References: [1]. Evans GB, et al. Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89. |
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| Cas No. | 653592-04-2 | SDF | |
| 别名 | MTDIA; Methylthio-DADMe-Immucillin A | ||
| Canonical SMILES | O[C@H]1CN(CC2=CNC3=C(N)N=CN=C32)C[C@@H]1CSC | ||
| 分子式 | C13H19N5OS | 分子量 | 293.39 |
| 溶解度 | DMSO : ≥ 33.33 mg/mL (113.60 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4084 mL | 17.0422 mL | 34.0843 mL |
| 5 mM | 0.6817 mL | 3.4084 mL | 6.8169 mL |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4084 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet